Open Access
Open access
volume 15 issue 4 pages 444

Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core

Egor V Savin 2
Michael D Tsymliakov 1
Anita I Maksutova 1
Victoria Yu Savitskaya 1
Sergey E Sosonyuk 1
Yulia A. Gracheva 1
Michael Yu Seliverstov 1
Natalia A Lozinskaya 1
Gelina S Kopeina 2
Publication typeJournal Article
Publication date2022-04-02
scimago Q1
wos Q1
SJR1.019
CiteScore7.7
Impact factor4.8
ISSN14248247
PubMed ID:  35455441
Drug Discovery
Pharmaceutical Science
Molecular Medicine
Abstract

The use of p53-MDM2 inhibitors is a prospective strategy in anti-cancer therapy for tumors expressing wild type p53 protein. In this study, we have applied a simple approach of two-step synthesis of imidazoline-based alkoxyaryl compounds, which are able to efficiently inhibit p53-MDM2 protein–protein interactions, promote accumulation of p53 and p53-inducible proteins in various cancer cell lines. Compounds 2l and 2k cause significant upregulation of p53 and p53-inducible proteins in five human cancer cell lines, one of which possesses overexpression of MDM2.

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GOST |
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GOST Copy
Bazanov D. R. et al. Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core // Pharmaceuticals. 2022. Vol. 15. No. 4. p. 444.
GOST all authors (up to 50) Copy
Bazanov D. R., Pervushin N. V., Savin E. V., Tsymliakov M. D., Maksutova A. I., Savitskaya V. Yu., Sosonyuk S. E., Gracheva Y. A., Seliverstov M. Yu., Lozinskaya N. A., Kopeina G. S. Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core // Pharmaceuticals. 2022. Vol. 15. No. 4. p. 444.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.3390/ph15040444
UR - https://www.mdpi.com/1424-8247/15/4/444
TI - Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core
T2 - Pharmaceuticals
AU - Bazanov, Daniil R
AU - Pervushin, Nikolay V
AU - Savin, Egor V
AU - Tsymliakov, Michael D
AU - Maksutova, Anita I
AU - Savitskaya, Victoria Yu
AU - Sosonyuk, Sergey E
AU - Gracheva, Yulia A.
AU - Seliverstov, Michael Yu
AU - Lozinskaya, Natalia A
AU - Kopeina, Gelina S
PY - 2022
DA - 2022/04/02
PB - MDPI
SP - 444
IS - 4
VL - 15
PMID - 35455441
SN - 1424-8247
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2022_Bazanov,
author = {Daniil R Bazanov and Nikolay V Pervushin and Egor V Savin and Michael D Tsymliakov and Anita I Maksutova and Victoria Yu Savitskaya and Sergey E Sosonyuk and Yulia A. Gracheva and Michael Yu Seliverstov and Natalia A Lozinskaya and Gelina S Kopeina},
title = {Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core},
journal = {Pharmaceuticals},
year = {2022},
volume = {15},
publisher = {MDPI},
month = {apr},
url = {https://www.mdpi.com/1424-8247/15/4/444},
number = {4},
pages = {444},
doi = {10.3390/ph15040444}
}
MLA
Cite this
MLA Copy
Bazanov, Daniil R., et al. “Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core.” Pharmaceuticals, vol. 15, no. 4, Apr. 2022, p. 444. https://www.mdpi.com/1424-8247/15/4/444.